Interleukin-1 (IL-1) receptor antagonist binds to the 80-kDa IL-1 receptor but does not initiate IL-1 signal transduction.

Interleukin-1 (IL-1) receptor antagonist binds to the 80-kDa IL-1 receptor but does not initiate IL-1 signal transduction.
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白介素 1 (IL-1) 受体拮抗剂与 80-kDa IL-1 受体结合,但不启动 IL-1 信号转导。

DOI:
10.1016/s0021-9258(18)99230-6
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发表时间:
1991
期刊:
The Journal of biological chemistry
影响因子:
--
通讯作者:
S. P. Eisenberg
S. P. Eisenberg
中科院分区:
--
文献类型:
--
作者:
D. Dripps;B. Brandhuber;R. Thompson;S. P. Eisenberg

文献摘要

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白细胞介素-1 受体拮抗剂 (IL-1ra) 是一种能够抑制 IL-1 受体结合和生物活性而不诱导 IL-1 样反应的蛋白质。平衡结合和动力学实验表明,IL-1ra 与小鼠胸腺瘤细胞系 EL4 上的 80 kDa IL-1 受体结合,亲和力 (KD = 150 pM) 大约等于 IL-1 α 和 IL-1 β 对该受体的亲和力。然而,IL-1ra 无法诱导与 IL-1 活性相关的两个早期事件。表面结合的 IL-1ra 不会经历受体介导的内化,并且 IL-1ra 不会激活负责下调小鼠 3T3 成纤维细胞系上 EGF 受体的蛋白激酶活性。未能诱导 IL-1 特有的一般性早期反应表明 IL-1ra 不太可能在任何表达 80-kDa 受体的细胞上充当激动剂。
The interleukin-1 receptor antagonist (IL-1ra) is a protein capable of inhibiting receptor binding and biological activities of IL-1 without inducing an IL-1-like response. Equilibrium binding and kinetic experiments show that IL-1ra binds to the 80-kDa IL-1 receptor on the murine thymoma cell line EL4 with an affinity (KD = 150 pM) approximately equal to that of IL-1 alpha and IL-1 beta for this receptor. However, IL-1ra is unable to induce two early events associated with IL-1 activity. Surface-bound IL-1ra does not undergo receptor-mediated internalization, and IL-1ra does not activate the protein kinase activity responsible for down-modulation of the EGF receptor on the murine 3T3 fibroblast cell line. The failure to induce general, early responses characteristic of IL-1 indicates that IL-1ra is unlikely to act as an agonist on any cell expressing the 80-kDa receptor.